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Abstract

Introduction:
Multidrug resistance remains a major obstacle hindering
successful antimalarial chemotherapy. In the current study, 50% metha
-
nol in dichloromethane extract and six compounds from the stem bark of
Zanthoxylum gilletii
were explored for their antiplasmodial potential against
three strains of
Plasmodium falciparum
.
Materials and Methods:
The ex
-
tract was obtained by cold percolation using 50 % MeOH in CH
2
Cl
2
and
the antiplasmodial activities were assayed using a non–radioactive Malaria
SYBR Green I assay to determine a concentration that inhibits growth of
50% of parasites in culture (IC
50
).
Results and Discussion:
Chromato
-
graphic separation of the crude extract yielded six known compounds
including: one lignan, sesamin (
1
), an alkamide, fagaramide (
2
), three benzo
[
c
] phenanthridine alkaloids, 8–acetonyldihydrochelerythrine (
3
), dihydro
-
chelerythine (
4
), norchelerythrine (
5
) and one pentacyclic triterpenoid,
lupeol (
6
). The extract and sesamin (
1
) showed promising antiplasmodial
activities against the chloroquine resistant (W2), chloroquine sensitive (D6)
and 3D7 strains of
P. falciparum
, with IC
50
values of 2.52, 1.48 and 1.43 μg/mL
and 5.4, 9.1 and 8.3 μM, respectively. To the best of our knowledge, this is
the first report on antiplasmodial activities of the stem bark extract (50% MeOH in CH
2
Cl
2
) and compound
1
–
3
and
6
. Furthermore, three of the
isolated compounds;
1
,
3
,
6
are reported from this species for the first
time.
Conclusion:
The good antiplasmodial activities exhibited by the stem
bark of
Z. gilletii
against three different strains of
P. falciparum
may be
attributed to the presence of
1
-
3
exhibiting good activities against all
strains of
P. falciparum
.